title: Synthesis and preliminary pharmacological evaluation of N-2-(4-(4-(2-substitutedthiazol-4-yl) piperazin-1-yl)-2-oxoethyl)acetamides as novel atypical antipsychotic agents.
abstract: A series of N-2-(4-(4-(2-substitutedthiazol-4-yl) piperazin-1-yl)-2-oxoethyl)acetamides were synthesized in an effort to prepare novel atypical antipsychotic agents. The compounds were synthesized by either microwave irradiation technique or by conventional synthesis and were characterized by spectral data (IR, (1)H NMR, and MS) and the purity was ascertained by microanalysis. All the synthesized compounds were screened for their in vivo pharmacological activity in Swiss albino mice. D(2) antagonism studies were performed using climbing mouse assay model and 5-HT(2A) antagonism studies were performed using quipazine induced head twitches in mice. It was observed that none of the new chemical entities exhibited catalepsy. AG 3 was found to be the most active compound.
authors.affiliation: Chemistry Group, Birla Institute of Technology & Science, FDIII, Vidya Vihar, Pilani, Rajasthan 333 031, India. kvgcs@yahoo.com
authors.forename: K V G Chandra
authors.initials: KV
authors.lastname: Sekhar
authors.forename: V S
authors.initials: VS
authors.lastname: Rao
authors.forename: Ravi Kumar Vyas
authors.initials: RKV
authors.lastname: Devambatla
authors.forename: M Murali Krishna
authors.initials: MM
authors.lastname: Kumar
mesh_terms: D000081:Acetamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D014150:Antipsychotic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020650:Combinatorial Chemistry Techniques; D004195:Disease Models, Animal; D019416:Head Movements / Q000187:drug effects; D051379:Mice; D015394:Molecular Structure; D009043:Motor Activity / Q000187:drug effects; D010879:Piperazines / Q000138:chemical synthesis* / Q000302:isolation & purification / Q000494:pharmacology*; D011814:Quipazine / Q000494:pharmacology; D058830:Serotonin 5-HT2 Receptor Antagonists
chemical_list: D000081:Acetamides; D014150:Antipsychotic Agents; D010879:Piperazines; D058830:Serotonin 5-HT2 Receptor Antagonists; D011814:Quipazine